Science
Mechanism of Action
S-TERTIAPIN SP operates by delivering a derivative, Tertiapin-Q, which acts as a highly selective potassium channel blocker. This peptide targets and occludes the external conduction pore of various inward rectifier potassium channels (Kir), such as GIRK1, GIRK4, and ROMK1, as well as calcium-activated large conductance K+ channels (BK/MaxiK). This precise blockage modulates ion flow, thereby impacting cellular excitability and action potential dynamics.
Research
Clinical Evidence
Low confidenceN/A
Key findings
- 01 In vitro studies demonstrated Tertiapin-Q's ability to inhibit BK-type K+ channels in a use- and concentration-dependent manner in Xenopus oocytes and cultured mouse dorsal root ganglion (DRG) neurons, with significant block observed at 1-100 nM and complete block achieved above 100 nM with continuous stimulation.
- 02 High-affinity binding of Tertiapin-Q was observed with ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels, exhibiting Ki values of 1.3 nM and 13.3 nM, respectively.
- 03 Tertiapin-Q effectively inhibits calcium-activated large conductance BK potassium channels (KCa1.1) with an IC50 of approximately 5 nM.
Transparency
Dusting Analysis
No data available regarding 'dusting' properties or thresholds for S-TERTIAPIN SP in cosmetic applications.
The Formula
Formulation
Stability
S-TERTIAPIN SP, specifically its derivative Tertiapin-Q, exhibits enhanced stability compared to native tertiapin. This is attributed to a glutamine substitution at position 13, which prevents methionine oxidation and preserves its channel-blocking efficacy. For optimal stability, stock solutions should be stored sealed and moisture-free at -80°C for up to six months, or at -20°C for one month.
Safety
Safety Profile
Official safety assessments by CIR, SCCS, or FDA for S-TERTIAPIN SP or Tertiapin-Q in cosmetic contexts are currently unavailable. Preclinical observations indicate potential neurotoxicity to dorsal root ganglion neurons when Tertiapin-Q is applied at high concentrations (exceeding 100 nM) for durations over 25 minutes under continuous stimulation.
Your Skin
Skin Compatibility
Our Assessment
Verdict
While demonstrating potent and precise potassium channel blocking activity in cellular models, S-TERTIAPIN SP currently lacks sufficient data regarding its specific cosmetic efficacy and comprehensive safety profile for skin application.
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